Sökning: WFRF:(Andreasson Joakim 1973)
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A Fluorescent Kinas...
A Fluorescent Kinase Inhibitor that Exhibits Diagnostic Changes in Emission upon Binding
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- Fleming, Cassandra, 1987 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology,Chalmers Univ Technol, Dept Chem & Chem Engn Phys Chem, S-41296 Gothenburg, Sweden.;Univ Gothenburg, Dept Chem & Mol Biol, S-41296 Gothenburg, Sweden.
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- Sandoz, Patrick A. (författare)
- KTH,Biofysik,Science for Life Laboratory, SciLifeLab
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- Inghardt, Tord (författare)
- AstraZeneca AB,AstraZeneca, Med Chem, Res & Early Dev Cardiovasc Renal & Metab, BioPharmaceut R&D, Gothenburg, Sweden.
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- Önfelt, Björn (författare)
- KTH,Science for Life Laboratory, SciLifeLab,Biomedicinsk fysik och röntgenfysik
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- Grötli, Morten, 1966 (författare)
- Gothenburg University,Göteborgs universitet,Institutionen för kemi och molekylärbiologi,Department of Chemistry and Molecular Biology,Univ Gothenburg, Dept Chem & Mol Biol, S-41296 Gothenburg, Sweden.
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- Andreasson, Joakim, 1973 (författare)
- Chalmers tekniska högskola,Chalmers University of Technology,Chalmers Univ Technol, Dept Chem & Chem Engn Phys Chem, S-41296 Gothenburg, Sweden.
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(creator_code:org_t)
- 2019-09-05
- 2019
- Engelska.
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Ingår i: Angewandte Chemie - International Edition. - : Wiley. - 1433-7851 .- 1521-3773. ; 58:42, s. 15000-15004
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Abstract
Ämnesord
Stäng
- The development of a fluorescent LCK inhibitor that exhibits favourable solvatochromic properties upon binding the kinase is described. Fluorescent properties were realised through the inclusion of a prodan-derived fluorophore into the pharmacophore of an ATP-competitive kinase inhibitor. Fluorescence titration experiments demonstrate the solvatochromic properties of the inhibitor, in which dramatic increase in emission intensity and hypsochromic shift in emission maxima are clearly observed upon binding LCK. Microscopy experiments in cellular contexts together with flow cytometry show that the fluorescence intensity of the inhibitor correlates with the LCK concentration. Furthermore, multiphoton microscopy experiments demonstrate both the rapid cellular uptake of the inhibitor and that the two-photon cross section of the inhibitor is amenable for excitation at 700 nm.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
- NATURVETENSKAP -- Fysik -- Atom- och molekylfysik och optik (hsv//swe)
- NATURAL SCIENCES -- Physical Sciences -- Atom and Molecular Physics and Optics (hsv//eng)
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
- NATURVETENSKAP -- Kemi (hsv//swe)
- NATURAL SCIENCES -- Chemical Sciences (hsv//eng)
Nyckelord
- solvatochromism
- kinase
- fluorescence
- inhibitors
- fluorescence
- inhibitors
- kinase
- solvatochromism
Publikations- och innehållstyp
- art (ämneskategori)
- ref (ämneskategori)
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